Preparation and in vitro evaluation of monoquaternary inhibitors of brain cholinesterases

Abstrakt

Acetylcholinesterase inhibitors are currently of high interest due to the many reasons. Among them, Alzheimer's disease drugs are of great interest.

In this study, eleven mono quarternary pyridinium salts substituted by different groups (electron donors and electron acceptors) in position four were prepared. Then, their anticholinesterase was tested.

As observed, their IC50 ranged from 33 µM to 3981 µM. Moreover, probability of blood-brain barrier penetration was predicted.